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α-Glucosidase inhibition of 6-hydroxyflavones. Part 3, Synthesis and evaluation of 2,3,4-trihydroxybenzoyl-containing flavonoid analogs and 6-aminoflavones as α-previous termglucosidasenext term inhibitors
Title: | α-Glucosidase inhibition of 6-hydroxyflavones. Part 3, Synthesis and evaluation of 2,3,4-trihydroxybenzoyl-containing flavonoid analogs and 6-aminoflavones as α-previous termglucosidasenext term inhibitors |
Authors: | Gao, Hong Browse this author | Kawabata, Jun2 Browse this author →KAKEN DB |
Authors(alt): | 川端, 潤2 |
Keywords: | α-previous termGlucosidase | structure-activity relationship | 6-hydroxyflavones | 6-aminoflavones |
Issue Date: | 1-Mar-2005 |
Publisher: | Elsevier |
Journal Title: | Bioorganic & Medicinal Chemistry |
Volume: | 13 |
Issue: | 5 |
Start Page: | 1661 |
End Page: | 1667 |
Publisher DOI: | 10.1016/j.bmc.2004.12.010 |
PMID: | 15698784 |
Abstract: | The SAR studies suggested that the C-ring of baicalein (1) was not necessary for the activity, and validated the importance of 2,3,4-trihydroxybenzoyl structure of 1. Thus, a series of 2,3,4-trihydroxybenzoyl-containing flavonoid analogs were investigated for the α-previous termglucosidasenext term inhibitory activity. The results indicated that 5,6,7-trihydroxy-2-phenyl-4-quinolone (2) and 5,6,7-trihydroxyflavanone (4) showed the comparable activity to 1, while 3,5,6,7-tetrahydroxyflavone (7), 5,6,7-trihydroxyisoflavone (8), and 6-hydroxygenistein (9) showed moderate α-previous termglucosidasenext term inhibitory activity. In addition, it was found that 6-amino-5,7-dihydroxyflavone (16) was a more potent and specific rat intestinal α-previous termglucosidasenext term inhibitor than 1, and showed the comparable activity to acarbose. This is the first report on mammalian intestinal α-previous termglucosidasenext term inhibitory activity of 6-aminoflavones. Kinetic studies revealed that 16 inhibited both sucrose- and maltose-hydrolyzing activities of rat intestinal α-previous termglucosidasenext term uncompetitively. |
Relation: | http://www.sciencedirect.com/science/journal/09680896 |
Type: | article (author version) |
URI: | http://hdl.handle.net/2115/433 |
Appears in Collections: | 農学院・農学研究院 (Graduate School of Agriculture / Faculty of Agriculture) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)
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Submitter: 川端 潤
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